Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitor
Explore this paper's citation graph
Summary
It is shown that resistance to PF00299804 arises, at least in part, through selection of a pre-existing EGFR T790M-amplified clone both in vitro and using a xenograft model in vivo and can be used to guide studies of patient tumor specimens from ongoing clinical trials of irreversible EGFR kinase inhibitors.
- Type
- article
- Published
- 2010-02-01
- Cited by
- 234
- References
- 47
- Access
- Open access
- OpenAlex
- https://openalex.org/W2040575339
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:6897145
Keywords
T790M, Gefitinib, Erlotinib, Cancer research, EGFR inhibitors
References
- Amplification and loss of dihydrofolate reductase genes in a Chinese hamster ovary cell line
- A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient.
- Analysis of Epidermal Growth Factor Receptor Gene Mutation in Patients with Non–Small Cell Lung Cancer and Acquired Resistance to Gefitinib
- Modeling oncogene addiction using RNA interference
- MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation.
- MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling
- Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification
- EGFR mutation and resistance of non-small-cell lung cancer to gefitinib.
- Hematologic and cytogenetic responses to imatinib mesylate in chronic myelogenous leukemia.
- A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome.
- Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia.
- Therapeutic Options Against BCR-ABL1 T315I-Positive Chronic Myelogenous Leukemia
- Allele-dependent variation in the relative cellular potency of distinct EGFR inhibitors
- 203 POSTER Neratinib (HKI-272), an irreversible pan-ErbB receptor tyrosine kinase inhibitor: preliminary results of a phase 2 trial in patients with advanced non-small cell lung cancer
- Gene amplification and drug resistance in cultured murine cells.
- Oncogenic activity of epidermal growth factor receptor kinase mutant alleles is enhanced by the T790M drug resistance mutation.
- ErbB-3 mediates phosphoinositide 3-kinase activity in gefitinib-sensitive non-small cell lung cancer cell lines.
- BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models
- Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer.
- Sorafenib Inhibits the Imatinib-Resistant KITT670I Gatekeeper Mutation in Gastrointestinal Stromal Tumor
Cited by
- Gefitinib resistance of cancer cells correlated with TM4SF5-mediated epithelial-mesenchymal transition.
- Apoptosis in targeted therapy responses: the role of BIM.
- Current drugs and drug targets in non-small cell lung cancer: limitations and opportunities.
- Investigation of positron emission tomography for pharmacological assessment of epidermal growth factor receptor-directed therapies
- Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.
- Pattern of Failure Analysis in Metastatic EGFR-Mutant Lung Cancer Treated with Tyrosine Kinase Inhibitors to Identify Candidates for Consolidation Stereotactic Body Radiation Therapy
- Circulating DNA as a Biomarker for Early Detection of Cancer: A Brief Update with an Emphasis on Lung Cancer~!2010-06-09~!2010-08-03~!2010-09-06~!
- Personalisierte medikamentöse Therapie des fortgeschrittenen nichtkleinzelligen Lungenkarzinoms
- Resistance to receptor tyrosine kinase inhibition in cancer: molecular mechanisms and therapeutic strategies
- Anti-HER3 monoclonal antibody patritumab sensitizes refractory non-small cell lung cancer to the epidermal growth factor receptor inhibitor erlotinib
- Understanding acquired resistance to Lapatinib in breast cancer cells
- Regulation of EGF receptor dynamics by protein tyrosine phosphatases
- The Receptor AXL Diversifies EGFR Signaling and Limits the Response to EGFR-Targeted Inhibitors in Triple-Negative Breast Cancer Cells
- NF-κB drives acquired resistance to a novel mutant-selective EGFR inhibitor
- Detection of low‐level EGFR T790M mutation in lung cancer tissues
- Signaling and Feedback Networks Underlying Senstivity and Resistance to Kinase Inhibitors in Oncogene Addicted Cancers
- Cancer Imaging Training in the 21st Century: An Overview of Where We Are, and Where We Need To Be.
- Mutational and network level mechanisms underlying resistance to anti-cancer kinase inhibitors.
- Erlotinib Resistance in Lung Cancer: Current Progress and Future Perspectives
- Lung cancer genotype-based therapy and predictive biomarkers: present and future.
Related papers
- Comparison of the therapeutic outcome between gefitinib and erlotinib in female patients with non-small-cell lung cancer
- Gefitinib or erlotinib in the treatment of advanced non-small cell lung cancer.
- Successful treatment of non-small cell lung cancer with gefitinib after severe erlotinib-related hepatotoxicity.
- Erlotinib as a salvage treatment for patients with advanced non-small cell lung cancer after failure of gefitinib treatment
- Erlotinib is a well-tolerated alternate treatment for non-small cell lung cancer in cases of gefitinib-induced hepatotoxicity.
- [Gefitinib versus Erlotinib as first-line treatment for patients with advanced EGFR mutation-positive non-small-cell lung cancer].
- Comparison of the efficacy of gefitinib and erlotinib as a second line treatment for advanced non-small cell lung cancer
- Long-term survival of non-small-cell lung cancer patients with EGFR inhibitor treatment.
- Sequential responses of adenocarcinoma of the lung to erlotinib after gefitinib in never smoker Korean woman.
- Challenges of detecting EGFR T790M in gefitinib/erlotinib-resistant tumours.